CP-31398-生命科學試劑-MCE

Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemECP-31398Cat.No.:HY-18343CASNo.:259199-65-0分子式:C??H??N?O分子量:362.47作用靶點:MDM-2/p53;Apoptosis作用通路:Apoptosis儲存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性CP-31398可在p53突變或野生型的癌細胞中，穩(wěn)定p53的活性構象，促進p53的活性。此外，CP-31398可上調(diào)p53目標基因，如p21WAF1/Cip1和KILLER/DR5。CP-31398具有抑制腫瘤生長的作用[1][2][3]。體外研究CP-31398(36.75μM,16h)inducesp21inp53-mutantcells[1].CP-31398(15μg/mL,20hours)couldinduceapoptosisandcellcyclearrestinSW480cells[2].WesternBlotAnalysis[1]CellLine:Saos-2cellsexpressingtransfectedmutantp53Concentration:36.75μMIncubationTime:16hResult:Inductionofp21incellsexpressingonlymutantp53.WesternBlotAnalysis[3]CellLine:LN-18andU87MGcellsConcentration:36μMIncubationTime:16hResult:Decreasedthelevelsofprocaspase3andinducedcleavageofcaspase7.1/2 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemE體內(nèi)研究CP-31398(100mg/kg,orally,twicedailyfor7days)exhibitssignificantanti-tumoractivityinmicemodels[1]AnimalModel:Smallhumantumorxenograftsinmice[1]Dosage:100mg/kgAdministration:Orallytwicedailyfor7daysResult:SuppressedA375.S2tumorgrowthby-50%.REFERENCESBAFoster,etal.Pharmacologicalrescueofmutantp53conformationandfunction.Science.1999Dec24;286(5449):2507-10.RishuTakimoto,etal.TheMutantp53-ConformationModifyingDrug,CP-31398,CanInduceApoptosisofHumanCancerCellsandCanStabilizeWild-Typep53Protein.CancerBiolTher.Jan-Feb2002;1(1):47-55.JWischhusen,etal.CP-31398,anovelp53-stabilizingagent,inducesp53-dependentandp53-independentgliomacelldeath.Oncogene.2003Nov13;22(51):8233-45.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-379